Any feedback?
Please rate this page
(literature.php)
(0/150)

BRENDA support

Literature summary for 5.6.2.1 extracted from

  • Peterson, K.E.; Cinelli, M.A.; Morrell, A.E.; Mehta, A.; Dexheimer, T.S.; Agama, K.; Antony, S.; Pommier, Y.; Cushman, M.
    Alcohol-, diol-, and carbohydrate-substituted indenoisoquinolines as topoisomerase I inhibitors: investigating the relationships involving stereochemistry, hydrogen bonding, and biological activity (2011), J. Med. Chem., 54, 4937-4953.
    View publication on PubMedView publication on EuropePMC
Search for more literature for 5.6.2.1

Inhibitors

Inhibitors Comment Organism Structure
1,5-dideoxy-1-(5,11-dioxo-5,11-dihydro-6H-indeno[1,2-c]isoquinolin-6-yl)-D-xylo-hexitol
-
 Homo sapiens
1-deoxy-1-(3-nitro-5,11-dioxo-5,11-dihydro-6H-indeno[1,2-c]isoquinolin-6-yl)-D-glucitol
-
 Homo sapiens
1-deoxy-1-(5,11-dioxo-5,11-dihydro-6H-indeno[1,2-c]isoquinolin-6-yl)-D-allitol
-
 Homo sapiens
1-deoxy-1-(5,11-dioxo-5,11-dihydro-6H-indeno[1,2-c]isoquinolin-6-yl)-D-arabinitol
-
 Homo sapiens
1-deoxy-1-(5,11-dioxo-5,11-dihydro-6H-indeno[1,2-c]isoquinolin-6-yl)-D-galactitol
-
 Homo sapiens
1-deoxy-1-(5,11-dioxo-5,11-dihydro-6H-indeno[1,2-c]isoquinolin-6-yl)-D-glucitol
-
 Homo sapiens
1-deoxy-1-(5,11-dioxo-5,11-dihydro-6H-indeno[1,2-c]isoquinolin-6-yl)-D-mannitol
-
 Homo sapiens
1-deoxy-1-(5,11-dioxo-5,11-dihydro-6H-indeno[1,2-c]isoquinolin-6-yl)-D-ribitol
-
 Homo sapiens
2,3-dimethoxy-6-methyl-5H-[1,3]dioxolo[5,6]indeno[1,2-c]isoquinoline-5,12(6H)-dione
-
 Homo sapiens
5-deoxy-5-(5,11-dioxo-5,11-dihydro-6H-indeno[1,2-c]isoquinolin-6-yl)-D-arabinitol
-
 Homo sapiens
6-(1-hydroxypropan-2-yl)-5H-indeno[1,2-c]isoquinoline-5,11(6H)-dione
-
 Homo sapiens
6-(2,3-dihydroxypropyl)-5H-indeno[1,2-c]isoquinoline-5,11(6H)-dione
-
 Homo sapiens
6-(2-hydroxypropyl)-5H-indeno[1,2-c]isoquinoline-5,11(6H)-dione
-
 Homo sapiens
6-(3-amino-2-hydroxypropyl)-5H-indeno[1,2-c]isoquinoline-5,11(6H)-dione
-
 Homo sapiens
6-(3-hydroxy-2-oxopropyl)-5H-indeno[1,2-c]isoquinoline-5,11(6H)-dione
-
 Homo sapiens
6-[(2R)-1-hydroxypropan-2-yl]-5H-indeno[1,2-c]isoquinoline-5,11(6H)-dione
-
 Homo sapiens
6-[(2R)-2,3-dihydroxypropyl]-5H-indeno[1,2-c]isoquinoline-5,11(6H)-dione
-
 Homo sapiens
6-[(2R)-2-hydroxypropyl]-5H-indeno[1,2-c]isoquinoline-5,11(6H)-dione
-
 Homo sapiens
6-[(2S)-1-hydroxypropan-2-yl]-5H-indeno[1,2-c]isoquinoline-5,11(6H)-dione
-
 Homo sapiens
6-[(2S)-2,3-dihydroxypropyl]-2,3-dimethoxy-5H-indeno[1,2-c]isoquinoline-5,11(6H)-dione
-
 Homo sapiens
6-[(2S)-2,3-dihydroxypropyl]-5H-indeno[1,2-c]isoquinoline-5,11(6H)-dione
-
 Homo sapiens
6-[(2S)-2-hydroxypropyl]-5H-indeno[1,2-c]isoquinoline-5,11(6H)-dione
-
 Homo sapiens
6-[3-(1H-imidazol-1-yl)propyl]-2,3-dimethoxy-5H-[1,3]dioxolo[5,6]indeno[1,2-c]isoquinoline-5,12(6H)-dione
-
 Homo sapiens
6-[3-[(2-hydroxyethyl)amino]propyl]-2,3-dimethoxy-5H-[1,3]dioxolo[5,6]indeno[1,2-c]isoquinoline-5,12(6H)-dione
-
 Homo sapiens
camptothecin
-
 Homo sapiens
additional information Top1 can be inhibited by heterocyclic compounds such as indolocarbazoles and indenoisoquinolines. Carbohydrate and hydroxyl-containing side chains are essential for the biological activity of indolocarbazoles. Preparation and inhibitory potency of indenoisoquinolines substituted with short-chain alcohols, diols, and carbohydrates, cytotoxicity, Top1 poisoning activity of diol-substituted indenoisoquinolines is dependent upon stereochemistry, molecular modeling, docking studies, and structure-function relationships, overview. IC50 values for cytotoxic effects in human cancer cell lines, overview Homo sapiens

Metals/Ions

Metals/Ions Comment Organism Structure
Mg2+ required Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Source Tissue

Source Tissue Comment Organism Textmining
commercial preparation recombinant enzyme Homo sapiens
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
additional information usage of a 3'-end radiolabeled DNA substrate, a 117-bp DNA oligonucleotide Homo sapiens ?
-
 ?

Synonyms

Synonyms Comment Organism
Top1
-
 Homo sapiens
Topoisomerase I
-
 Homo sapiens

Temperature Optimum [°C]

Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
25
-
 assay at Homo sapiens

pH Optimum

pH Optimum Minimum pH Optimum Maximum Comment Organism
7.5
-
 assay at Homo sapiens